CAS NO: | 603-00-9 |
包装 | 价格(元) |
10mM (in 1mL DMSO) | 电议 |
1g | 电议 |
5g | 电议 |
10g | 电议 |
Cas No. | 603-00-9 |
别名 | 羟丙茶碱 |
化学名 | 3,7-dihydro-7-(2-hydroxypropyl)-1,3-dimethyl-1H-purine-2,6-dione |
Canonical SMILES | CN(C(N1C)=O)C2=C(N(CC(O)C)C=N2)C1=O |
分子式 | C10H14N4O3 |
分子量 | 238.2 |
溶解度 | ≥ 10.1mg/mL in DMSO |
储存条件 | Store at -20℃ |
General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
Shipping Condition | Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request |
产品描述 | Ki: 82 nM for bovine brain A1 adenosine receptor Proxyphylline is an A1 adenosine receptor antagonist. The A1 adenosine receptor, the best characterized purinergic receptor family, can mediate responses via multiple pertussis toxin-sensitive GTP binding proteins to various different effectors. In vitro: Previous study showed that proxyphylline could selectively antagonize A1 adenosine receptors versus A2 adenosine receptors (Ki = 850 μM for platelets) [1]. In vivo: In a previous study, rats that were allodynic following the vincristine injections were randomly allocated into four groups. Theoesberiven F (a combination of proxyphylline and Melilotus extract) was administered to rats. Results showed that the decreased paw withdrawal threshold induced by vincristine injection was increased by theoesberiven F treatment and the increased withdrawal frequency to cold stimuli was also reduced by theoesberiven F treatment [2]. Clinical trial: The proxyphylline PK was measured in healthy adults after intravenous, single oral and multiple oral doses to produce steady state. The mean peak time after oral administration was 29 min. The apparent volume of distribution was 0.611/kg. The ranges of biological half-life were 8.1-12.1 h and 8.3-12.6 h calculated from serum and urine data, respectively. In additioin, 24% of the dose was excreted in urine, which agreed with the relationship between the calculated total body clearance and the renal clearance of the drug [3]. References: |